Department of Pharmaceutical Technology, Jadavpur University, Kolkata, 700032, India.
Department of Chemical and Biomolecular Engineering, Chonnam National University, Jeonnam, Yeosu, 59626, South Korea.
AAPS PharmSciTech. 2024 Jul 12;25(6):162. doi: 10.1208/s12249-024-02874-y.
In 1987, Won invented the solid-phase porous microsphere (MS), which stores bioactive compounds in many interconnected voids. Spherical particles (5-300 μm), MS, may form clusters of smaller spheres, resulting in many benefits. The current investigation focussed on gel-encased formulation, which can be suitable for dermal usage. First, quasi-emulsion (w/o/w) solvent evaporation was used to prepare 5-fluorouracil (5 FU) MS particles. The final product was characterized (SEM shows porous structure, FTIR and DSC showed drug compatibility with excipients, and gel formulation is shear-thinning) and further scaled up using the 8-fold method. Furthermore, CCD (Central Composite Design) was implemented to obtain the optimized results. After optimizing the conditions, including the polymer (600 mg, ethyl cellulose (EC), eudragit RS 100 (ERS)), stirring speed (1197 rpm), and surfactant concentration (2% w/v), we achieved the following results: optimal yield (63%), mean particle size (152 µm), drug entrapment efficiency (76%), and cumulative drug release (74.24% within 8 h). These findings are promising for industrial applications and align with the objectives outlined in UN Sustainable Development Goals 3, 9, and 17, as well as the goals of the G20 initiative.
1987 年，Won 发明了固相多孔微球（MS），它将生物活性化合物储存在许多相互连接的空隙中。球形颗粒（5-300μm），MS，可能会形成较小球体的簇，从而带来许多好处。目前的研究集中在凝胶包封配方上，它可能适用于皮肤使用。首先，采用拟乳液（w/o/w）溶剂蒸发法制备 5-氟尿嘧啶（5FU）MS 颗粒。最终产物进行了特征描述（SEM 显示多孔结构，FTIR 和 DSC 显示药物与赋形剂的相容性，凝胶配方具有剪切变稀性），并使用 8 倍方法进一步放大。此外，还实施了 CCD（中心复合设计）以获得优化结果。在优化条件后，包括聚合物（600mg，乙基纤维素（EC），Eudragit RS 100（ERS））、搅拌速度（1197rpm）和表面活性剂浓度（2%w/v），我们得到了以下结果：最佳收率（63%）、平均粒径（152μm）、药物包封效率（76%）和累积药物释放（8h 内 74.24%）。这些发现有望在工业应用中得到应用，符合联合国可持续发展目标 3、9 和 17 以及 20 国集团倡议的目标。
